dimethylthexyl siloxytecan

Dimethylthexyl siloxytecan is a silylated analog of SN-38, the active metabolite of the chemotherapy drug irinotecan. Developed as part of a series of siloxytecans, this compound features a dimethylthexyl siloxy group that enhances lipophilicity and metabolic stability while providing intrinsic blue-fluorescent properties. This fluorescence enables real-time, quantitative visualization of intracellular uptake and distribution without the need for external labels or extensive sample preparation. Mechanistically, it acts as a potent topoisomerase I inhibitor, inducing G2 cell cycle arrest and apoptosis in cancer cells. Preclinical evaluations have shown superior potency and cellular uptake compared to parent compounds, with significant activity observed in models of colorectal, triple-negative breast, ovarian, non-small cell lung, and liver cancers. Its exceptional tissue retention following direct injection makes it a promising candidate for localized cancer therapy and in vivo evaluation.

Other names

dimethylthexyl siloxy-SN-38